Medicinal preparation.



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PAUL EI-IRLICI-I AND ALFRED IBERTI-IEIIVI, OF FRANKFORT-ON-THE-MAIN, GERMANY,

ASSIGNORS TO FABIBWERKE VORM. MEISTER LUCIUS & BRUNING, F HUCHST-ON- THE-MAIN, GERMANY, A CORPORATION OF GERMANY.

MEDICINAL PREPARATION.

N0 Drawing. Application filed August 6, 1912, Serial No. 713.508. Renewed August 13, 1913.

Specification of Letters Patent.

Patented Dec. 1 6,191 3.

Serial No.

--As=As \mu/ l I l The aniino-ortyarsenobenzenes, and par 'ticularly the il -(lltHI1ln0- l:4'(lIOXXHISPIIO- benzene have been tound to be valuable I products .lor therapeutical purposes and especially for the trcati'nent of syphilis and all) other infectious diseases. The free bases, however, are insoluble or dithcultly soluble in water but they can be dissolved 1n alkalies to form salts and the can also be dissolved in dilute acids such as hydrocloric acid. The hydrochlorids or dihydrochlorids are readily soluble in water, and accordingly are a more advantageous form for use than the tree bases.

The present invention relates to alkaline solutions or neutral suspensions made from such hydrochlorids, and specifically to the alkaline solutions and suspensions made from the dihydrochlorids of the 23Sdiarnino-tQ-dioxarsenobenzene, these solutions or suspensions being suitable and advantageous for hypodermic injections.

The invention will be further described in connection with the dihydrocl'ilorid oi the 3-3-diaminol- -dioxyarsenobenzene, hcrcinafter referred to as the dihydrochlorid.

The following procedure gives a solution suitable for intravenous injection. la grains of chemically pure sodium hydroxid are dissolved in 8.5 c. c. distilled water. For 0.5 gram at the dihydrochlorid 1.00 grams equal to about 0.95 c. 0. equal to about 1920 drops of this solution are used. Into a narrow-necked graduated glass stopperccl sterile cylindcr-mcasure of 300 c. (3. capacity, containing about 50 sterile glass beads 30 to 4-0 c. c. sterile distilled water is measured. Then the dihydrochlorid e. 9., 0.5 ,Q'lfllll is adckrd, and shaken until it goes entirely into solution and the solution does not show, even when examined by transmitted light, any gelatinous dr(' p-like particles. After solution is completed, and the solution is clear and free from undissolvcd particles, 10 drops of the 15% caustic soda solution already described are added all atoncc. The precipitate at first termed, dissolves on shaking and there results a clear yellow so lution. This solution is diluted to 250 c. c. with sterile 0.5% saline solution which has been prepared :trom chemically pure sodium chlorid and sterile distilled water, treshly prepared. lln case the solution is not quite clear, or becomes slightly turbid atter a tow minutes, a few more drops of caustic soda solution should be added, a drop at a time and waiting: 2 or minutes al'tcr each drop to see it this quantity sullices to clear the solution. The resulting clear solution is ready for use. This solution contains 0.5 gram ol. the dihydroel'ilorid in 250 c. c. For less amounts of the dihydrochlorid, the corresponding amounts ol. the solution can be used. fl i'istcad of using the graduated glass cylinder, the concentrated solution of the dihydrochlorid can be prepared in a small glassstoppercd llask with the aid of glass beads, and a l ter the subsequent addition ol caustic soda solution and complete clarification, poured into the saline solution. A. solution for intrannlscular injection can also be made with the alkaline solution already described, but in this case a nmch smaller amount of: fluid (only about c. o.) is required. For its n'e1' aration, for exai'nple, 0.5 grain of the dihydrochlorid are well trituratcd in a sterile mortar with drops of the caustic soda solution, and then diluted with distilled water to the desired volume.

For subcutaneous injection it is sometimes advantageous to use neutral suspensions made from the dihydrochlorid. For this purpose the dihydrochlorid powder, 0. g. 0.5 gram, is introduced into a sterile porcelain dish, and triturated carefully with 8 drops (0.5 gra1n::0.380 c. c.) caustic soda solution. To it is added, at first drop by drop, with constant trituration, the requisite quantity (about to c. c.) sterile water. The fine suspension produced is tested with litmus paper eXact-issime for neutral reaction, a drop of caustic soda solution or of dilute hydrochloric acid being added if necessary.

The solution of caustic soda previously described can be used in making the various alkaline solutions as well as the neutral suspension according to the present invention.

What We claimand desire to secure by Letters Patent of the United States is 1. The process of producing a preparation of amino-oXy-arsenobenzenes which comprises treating such products in the form of their hydrochlorids with a solution of a caustic alkali.

2. The process of producing a preparation of amino oxy arsenobenzenes which comprises treating such products in the form of their hydrochlorids with a solution of caustic soda.

3. The process of producing a preparation of diamino-dioxy-arsenobenzenes which comprises treating such products in the form of their dihydrochlorids with a solution of 1 caustic alkali.

4. The process of producing a preparation of diamino-dioxy-arsenobenzenes which comprises treating such products in the form of their dihydrochlorids with a solution of caustic soda...

5. The process of producing a preparation of diamino-dioxy-arsenobenzenes which comprises treating such products in the form of their dihydrochlorids with a 15% solution of caustic soda.

6. The process of producing a preparation of 3 8- diamino 4: 4tdioxyarsenobenz'ene which comprises treating the same in the form of its dihydrochlorid with a 15% solution of caustic soda.

7. Analkaline injection preparation comprising an aminooxyarsenobenezene and caustic alkali.

8. An alkaline injectlon preparation comprising a polyamino-dioxyarsenobenzene and 'amidooxyarsenobenzene in a causticalkali.

'11. An alkaline injection preparation comprising a solution of hydrochlorid of a polyamino-dioXy-arsenobenzene in a caustic alkali.

12. An alkaline injection preparation comprising a solution of a hydrochlorid of a diamino-dioxyarsenobenzene in a caustic alkali.

13. An alkaline injection preparation comprising a solution of a dihydrochlorid of an aminooxyarsenobenzene in caustic soda.

14:. An alkaline injection preparation comprising a solution of a dihydrochlorid of a polyamino-dioxy-arsenobenzene and caustic alkali.

15. An alkaline injection preparation comprising a solution of a dihydrochlorid of a diamino-dioxy-arsenobenzene in caustic soda.

16. An alkaline injection preparation comprising the dihydrochlorid of 3-3'-diamine- L4,-dioxy-arsenobenzene dissolved in a caustic soda solution.

17. An alkaline injection preparation comprising the dihydrochlorid of 3-3-diam inc-t4-dioXy-arsenobenzene dissolved in a 15% caustic soda solution.

In testimony whereof we have hereunto signed our names in the presence of two subscribing witnesses.

PAUL EHRLTOH. ALFRED BERTHETM. Witnesses:

CARL GRUND. ELsE MEBUS. 

